Drug discovery and assay development in the ubiquitin-proteasome system

被引：16

作者：

Berkers, Celia R. ^{[1
]}

Ovaa, Huib ^{[1
]}

机构：

[1] Netherlands Canc Inst, Div Cell Biol, NL-1066 CX Amsterdam, Netherlands

来源：

BIOCHEMICAL SOCIETY TRANSACTIONS | 2010年 / 38卷

关键词：

bortezomib; cartilzomib; immunoproteasome inhibitor; mycobactericidal proteasome inhibitor; proteasome; proteasome activity assay; PEGYLATED LIPOSOMAL DOXORUBICIN; MULTIPLE-MYELOMA CELLS; INHIBITOR BORTEZOMIB; IN-VIVO; HEMATOLOGIC MALIGNANCIES; IRREVERSIBLE INHIBITOR; REGULATORY PARTICLE; PEPTOID INHIBITOR; CRYSTAL-STRUCTURE; 20S PROTEASOMES;

D O I：

10.1042/BST0380014

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

The observation that tumour cells are more sensitive to pharmacological inhibition of the proteasome than normal cells has led to the development of the proteasome inhibitor bortezomib. To date, this is the only proteasome inhibitor that has been approved for clinical use. The clinical success of bortezomib, combined with the occurrence of adverse effects and the development of clinical resistance against this compound, has initiated the development of a broad range of second-generation proteasome inhibitors as well as of assays that can be used to establish a relationship between the extent and type of proteasome inhibition and the effectiveness of a particular drug. in the present paper, we discuss new strategies that may be used in the future to overcome drug resistance and to broaden the use of proteasome inhibitors for the treatment of both cancer and infectious and autoimmune disease.

引用

页码：14 / 20

页数：7

共 47 条

[1] The development of proteasome inhibitors as anticancer drugs [J].

Adams, J .

CANCER CELL, 2004, 5 (05) :417-421

[2] Profiling proteasome activity in tissue with fluorescent probes [J].

Berkers, Celia R. ;

van Leeuwen, Fijs W. B. ;

Groothuis, Tom A. ;

Peperzak, Victor ;

van Tilburg, Erica W. ;

Borst, Jannie ;

Neefjes, Jacques J. ;

Ovaa, Huib .

MOLECULAR PHARMACEUTICS, 2007, 4 (05) :739-748

[3] Activity probe for in vivo profiling of the specificity of proteasome inhibitor bortezomib [J].

Berkers, CR ;

Verdoes, M ;

Lichtman, E ;

Fiebiger, E ;

Kessler, BM ;

Anderson, KC ;

Ploegh, HL ;

Ovaa, H ;

Galardy, PJ .

NATURE METHODS, 2005, 2 (05) :357-362

[4] A novel orally active proteasome inhibitor induces apoptosis in multiple myeloma cells with mechanisms distinct from Bortezomib [J].

Chauhan, D ;

Catley, L ;

Li, GL ;

Podar, K ;

Hideshima, T ;

Velankar, M ;

Mitsiades, C ;

Mitsiades, N ;

Yasui, H ;

Letai, A ;

Ovaa, H ;

Berkers, C ;

Nicholson, B ;

Chao, TH ;

Neuteboom, STC ;

Richardson, P ;

Palladino, MA ;

Anderson, KC .

CANCER CELL, 2005, 8 (05) :407-419

[5]

Chauhan D, 2008, BLOOD, V111, P1654, DOI 10.1182/blood-2006-10-050476

[6] Targeting the UPS as therapy in multiple myeloma [J].

Chauhan, Dharminder ;

Bianchi, Giada ;

Anderson, Kenneth C. .

BMC BIOCHEMISTRY, 2008, 9

[7] Different proteasome subtypes in a single tissue exhibit different enzymatic properties [J].

Dahlmann, B ;

Ruppert, T ;

Kuehn, L ;

Merforth, S ;

Kloetzel, PM .

JOURNAL OF MOLECULAR BIOLOGY, 2000, 303 (05) :643-653

[8] Subtypes of 20S proteasomes from skeletal muscle [J].

Dahlmann, B ;

Ruppert, T ;

Kloetzel, PM ;

Kuehn, L .

BIOCHIMIE, 2001, 83 (3-4) :295-299

[9] Short-lived green fluorescent proteins for quantifying ubiquitin/proteasome-dependent proteolysis in living cells [J].

Dantuma, NP ;

Lindsten, K ;

Glas, R ;

Jellne, M ;

Masucci, MG .

NATURE BIOTECHNOLOGY, 2000, 18 (05) :538-543

[10] Antitumor activity of PR-171, a novel irreversible inhibitor of the proteasome [J].

Demo, Susan D. ;

Kirk, Christopher J. ;

Aujay, Monette A. ;

Buchholz, Tonia J. ;

Dajee, Maya ;

Ho, Mark N. ;

Jiang, Jing ;

Laidig, Guy J. ;

Lewis, Evan R. ;

Parlati, Francesco ;

Shenk, Kevin D. ;

Smyth, Mark S. ;

Sun, Congcong M. ;

Vallone, Marcy K. ;

Woo, Tina M. ;

Molineaux, Christopher J. ;

Bennett, Mark K. .

CANCER RESEARCH, 2007, 67 (13) :6383-6391

← 1 2 3 4 5 →